EP2363128A3 - Indol-Modulatoren von ATP-bindenden Kassetten-Transportern - Google Patents

Indol-Modulatoren von ATP-bindenden Kassetten-Transportern Download PDF

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Publication number
EP2363128A3
EP2363128A3 EP10185335A EP10185335A EP2363128A3 EP 2363128 A3 EP2363128 A3 EP 2363128A3 EP 10185335 A EP10185335 A EP 10185335A EP 10185335 A EP10185335 A EP 10185335A EP 2363128 A3 EP2363128 A3 EP 2363128A3
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EP
European Patent Office
Prior art keywords
modulators
atp
binding cassette
indole
cassette transporters
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP10185335A
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English (en)
French (fr)
Other versions
EP2363128A2 (de
EP2363128B1 (de
Inventor
Ruah Sara Hadida
Anna R. Halzewood
Peter D. J. Grootenhuis
Jinglan Zhou
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of EP2363128A2 publication Critical patent/EP2363128A2/de
Publication of EP2363128A3 publication Critical patent/EP2363128A3/de
Application granted granted Critical
Publication of EP2363128B1 publication Critical patent/EP2363128B1/de
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/20Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals substituted additionally by nitrogen atoms, e.g. tryptophane
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A61P5/16Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychology (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
EP10185335.6A 2005-03-11 2006-03-13 Indol-Modulatoren von ATP-bindenden Kassetten-Transportern Active EP2363128B1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US66131005P 2005-03-11 2005-03-11
US66917405P 2005-04-07 2005-04-07
EP06737945A EP1865949B1 (de) 2005-03-11 2006-03-13 Modulatoren von ATP-bindenden Kassettentransportern

Related Parent Applications (2)

Application Number Title Priority Date Filing Date
EP06737945A Division EP1865949B1 (de) 2005-03-11 2006-03-13 Modulatoren von ATP-bindenden Kassettentransportern
EP06737945.3 Division 2006-03-13

Publications (3)

Publication Number Publication Date
EP2363128A2 EP2363128A2 (de) 2011-09-07
EP2363128A3 true EP2363128A3 (de) 2011-09-21
EP2363128B1 EP2363128B1 (de) 2016-02-17

Family

ID=36869878

Family Applications (2)

Application Number Title Priority Date Filing Date
EP06737945A Active EP1865949B1 (de) 2005-03-11 2006-03-13 Modulatoren von ATP-bindenden Kassettentransportern
EP10185335.6A Active EP2363128B1 (de) 2005-03-11 2006-03-13 Indol-Modulatoren von ATP-bindenden Kassetten-Transportern

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EP06737945A Active EP1865949B1 (de) 2005-03-11 2006-03-13 Modulatoren von ATP-bindenden Kassettentransportern

Country Status (4)

Country Link
US (3) US8242149B2 (de)
EP (2) EP1865949B1 (de)
JP (2) JP5385605B2 (de)
WO (1) WO2006099256A2 (de)

Families Citing this family (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100074949A1 (en) 2008-08-13 2010-03-25 William Rowe Pharmaceutical composition and administration thereof
KR20060088537A (ko) 2003-09-06 2006-08-04 버텍스 파마슈티칼스 인코포레이티드 Atp-결합 카세트 수송체의 조절자
JP4869072B2 (ja) * 2003-11-14 2012-02-01 バーテックス ファーマシューティカルズ インコーポレイテッド Atp結合カセットトランスポーターのモジュレーターとして有用なチアゾールおよびオキサゾール
US7977322B2 (en) 2004-08-20 2011-07-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
CN101006076B (zh) 2004-06-24 2010-09-29 沃泰克斯药物股份有限公司 Atp-结合弹夹转运蛋白的调控剂
AU2006279810B2 (en) 2005-08-11 2011-10-27 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP2404919B1 (de) 2005-11-08 2013-08-21 Vertex Pharmaceuticals Incorporated Heterozyklische Verbindung zur Verwendung als Modulator von ATP-bindenden Kassettentransportern
DK3219705T3 (da) 2005-12-28 2020-04-14 Vertex Pharma Farmaceutiske sammensætninger af den amorfe form af n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinolin-3-carboxamid
JP5165586B2 (ja) 2005-12-28 2013-03-21 バーテックス ファーマシューティカルズ インコーポレイテッド 嚢胞性線維症の処置のためのATP結合カセットトランスポーターのモジュレーターとしての、1−(ベンゾ[d][1,3]ジオキソール−5−イル)−N−(フェニル)シクロプロパン−カルボキサミド誘導体および関連化合物
US7671221B2 (en) * 2005-12-28 2010-03-02 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
PL2007756T3 (pl) 2006-04-07 2016-01-29 Vertex Pharma Modulatory transporterów posiadających kasetę wiążącą ATP
US7645789B2 (en) 2006-04-07 2010-01-12 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
WO2008073623A2 (en) * 2006-11-02 2008-06-19 Arete Therapeutics, Inc. Soluble epoxide hydrolase inhibitors
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
ES2361595T3 (es) 2007-05-07 2011-06-20 Novartis Ag Compuestos orgánicos.
US8969386B2 (en) 2007-05-09 2015-03-03 Vertex Pharmaceuticals Incorporated Modulators of CFTR
WO2009038913A2 (en) 2007-08-24 2009-03-26 Vertex Pharmaceuticals Incorporated Isothiazolopyridinones useful for the treatment of (inter alia) cystic fibrosis
US20090099199A1 (en) * 2007-10-16 2009-04-16 Joachim Nozulak Organic compounds
EP2217572B1 (de) 2007-11-16 2013-11-06 Vertex Pharmaceuticals Incorporated Isochinoline als modulatoren von transportern der atp-bindenden kassette
EP2237768A2 (de) * 2007-12-07 2010-10-13 Vertex Pharmaceuticals Incorporated Formulierungen von 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropancarboxamid)-3-methylpyridin-2-yl)benzoesäure
US20100036130A1 (en) 2007-12-07 2010-02-11 Vertex Pharmaceuticals Incorporated Processes for producing cycloalkylcarboxamido-pyridine benzoic acids
MX364936B (es) 2007-12-07 2019-05-15 Vertex Pharma Procesos para producir acidos cicloalquilcarboxamido-piridin benzoicos.
PL2225230T3 (pl) 2007-12-07 2017-08-31 Vertex Pharmaceuticals Incorporated Stałe postacie kwasu 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-ilo)cyklopropanokarboksyamido)-3-metylopirydyn-2-ylo)benzoesowego
MX2010006421A (es) 2007-12-10 2010-06-25 Novartis Ag Compuestos organicos.
ES2647531T3 (es) 2008-02-28 2017-12-22 Vertex Pharmaceuticals Incorporated Derivados de heteroarilo como moduladores de CFTR
EP2271621B1 (de) 2008-03-31 2013-11-20 Vertex Pharmaceuticals Incorporated Pyridylderivate als cftr-modulatoren
BRPI0915018A2 (pt) 2008-06-10 2015-10-27 Novartis Ag compostos orgânicos
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EP2363128A2 (de) 2011-09-07
EP1865949B1 (de) 2012-11-14
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US20070264196A1 (en) 2007-11-15
US20140155626A1 (en) 2014-06-05
EP1865949A2 (de) 2007-12-19
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